The invention relates to hypoxic cell radiation sensitizers and cytotoxic agents which have high radiosensitizing activity and selective toxicity to hypoxic cells.
U.S. Pat. No. 4,603,133 relates to esters, amides and N-substituted amides of 2-[N-(morpholinoalkyl)aminosulfonyl]-6-nitrobenzoic acids, ued as sensitizers of hypoxic tumor cells to therapeutic radiation. That patent also relates to 2-chlorosulfonyl-6-nitrobenzoate ester prepared as described in U.S. Serial No. 716,886 filed Mar. 27, 1985 and aminating said 2-chlorosulfonylbenzoate ester to produce the corresponding sulfamyl or N-substituted sulfamylnitrobenzoic esters.
U.S. Ser. No. 937,275, filed Dec. 3, 1986, describes 3-nitrobenzenesulfonamides useful in enhancing the effect of therapeutic radiation.
U.S. Ser. No. 937,277, filed Dec. 3, 1986, describes 2-(substituted sulfamyl) derivatives of 4-nitrobenzamide useful for increasing the sensitivity of hypoxic cancer cells to X-rays and gamma-radiation.
U.S. Pat. No. 4,731,369 describes amides and esters of 2-(N-hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl)-aminosulfonyl)-6-nitrobenzoic acids which are useful for treating patients in need of therapeutic radiation.